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S81477

17-DMAG (Alvespimycin) HCl

源叶(MedMol) ≥98%
  • 英文名:
  • 17-DMAG (Alvespimycin) HCl
  • 别名:
  • NSC 707545;阿螺旋霉素盐酸盐
  • CAS号:
  • 467214-21-7
  • 分子式:
  • C32H48N4O8•HCl
  • 分子量:
  • 653.21
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S81477-25mg ≥98% ¥610.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S81477-100mg ≥98% ¥2270.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Alvespimycin hydrochloride (17-DMAG hydrochloride; KOS-1022; BMS 826476) is a potent inhibitor of Hsp90, binding to Hsp90 with EC50 of 62±29 nM.
  • 靶点: HSP90:62 nM (EC50);GRP94:65 nM (EC50);Apoptosis; HSP
  • 体内研究:
    The tumors are grown for two months before the start of i.p. injections every four days over one month with 0, 50, 100 and 200 mg/kg dipalmitoyl-radicicol or 0, 5, 10 and 20 mg/kg 17-DMAG. Despite sample heterogeneity, the HSP90 inhibitor-treated animals have significantly lower tumour volumes than the vehicle control-treated animals. HSP90 inhibitors have been shown to cause liver toxicity in an animal model of gastrointestinal cancer. Nevertheless, the reduction in tumor size using dipalmitoyl-radicicol is statistically significant at 100 mg/kg, while 17-DMAG at either 10 or 20 mg/kg elicited a significant reduction in tumor size
  • 参考文献:
    1. Ge J, et al. Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. J Med Chem. 2006 Jul 27;49(15):4606-15. 2. Hertlein E, et al. 17-DMAG targets the nuclear factor-kappaB family of proteins to induce apoptosis in chronic lymphocytic leukemia: clinical implications of HSP90 inhibition. Blood. 2010 Jul 8;116(1):45-53. 3. Henke A, et al. Reduced Contractility and Motility of Prostatic Cancer-Associated Fibroblasts after Inhibition of Heat Shock Protein 90. Cancers (Basel). 2016 Aug 24;8(9). pii: E77.
  • 溶解性: Soluble  in  DMSO、H2O
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.531 ml 7.655 ml 15.309 ml
    5 mM 0.306 ml 1.531 ml 3.062 ml
    10 mM 0.153 ml 0.765 ml 1.531 ml
    50 mM 0.031 ml 0.153 ml 0.306 ml
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